PF-04418948_1078166-57-0_DataSheet_MedChemExpress

Product Name:

PF-04418948CAS No.:

1078166-57-0Cat. No.:

HY-18966

Product Data Sheet

MWt:

409.41Formula:

C23H20FNO5Purity :>98%

Solubility:

10 mM in DMSO

Mechanisms:

Biological Activity:

PF-04418948is a novel,potent and selective prostaglandin EP2receptor antagonist with IC50of 16 Pathways:GPCR/G protein; Target:Prostaglandin Receptor PF 04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16nM, displays >2000-fold functional selectivity for the human EP2 receptor over antagonist activity

against the human EP1, EP3, EP4, DP1 and CRTH2 receptors.

IC50 value: 16 nM

Target: EP2in vitro: PF-04418948 inhibits prostaglandin E2 (PGE2)-induced increase in cAMP in cells expressing EP2 receptors with a functional KB value of 1.8 nM. In human myometrium, PF-

04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractions

induced by electrical field stimulation with an apparent KB of 5.4 nM. [1]References:

[1]. af Forselles KJ, et al. In vitro and in vivo characterization of PF-04418948, a novel, potent and

selective prostaglandin EP2 receptor antagonist. Br J Pharmacol. 2011 Dec;164(7):1847-1856.[2].Birrell MA,et al.Selectivity profiling of the novel EP2receptor antagonist,PF-04418948,in in vivo: In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of the PGE2-induced relaxation curve with a KB of 2.5 nM and an apparent KB of 1.3 nM respectively.Reversal of the PGE2-induced relaxation in the ...

[2]. Birrell MA, et al. Selectivity profiling of the novel EP2 receptor antagonist, PF 04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor. Br J Pharmacol. 2013

Jan;168(1):129-138.Caution: Not fully tested. For research purposes only

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